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Submit ReviewYIL 781 hydrochloride
Description: Ghrelin receptor (GHS-R1a) antagonist
Chemical Name: 6-(4-Fluorophenoxy)-2-methyl-3-[[(3S)-1-(1-methylethyl)-3-piperidinyl]methyl]-4(3H)-quinazolinone hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for YIL 781 hydrochloride
YIL 781 hydrochloride is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM). Displays no significant affinity for the motilin receptor (Ki = 6 μM). Blocks the effects of ghrelin on insulin secretion both in vivo and in vitro. Improves glucose homeostasis in vivo.
Compound Libraries for YIL 781 hydrochloride
YIL 781 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for YIL 781 hydrochloride
| M. Wt | 445.96 |
| Formula | C24H28FN3O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1640226-17-0 |
| PubChem ID | 74889155 |
| InChI Key | QQGRMONBDBMLSP-FERBBOLQSA-N |
| Smiles | O=C2C1=CC(OC4=CC=C(F)C=C4)=CC=C1N=C(C)N2C[C@@H]3CN(C(C)C)CCC3.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for YIL 781 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.6 | 100 | |
| water | 44.6 | 100 |
Preparing Stock Solutions for YIL 781 hydrochloride
The following data is based on the product molecular weight 445.96. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.24 mL | 11.21 mL | 22.42 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.48 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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Product Datasheets for YIL 781 hydrochloride
References for YIL 781 hydrochloride
References are publications that support the biological activity of the product.
Esler et al (2007) Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss. Endocrinology 148 5175 PMID: 17656463
Moran and Dailey (2009) Gut peptides: targets for antiobesity drug development? Endocrinology 150 2526 PMID: 19372201
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Keywords: YIL 781 hydrochloride, YIL 781 hydrochloride supplier, YIL781, YIL, 781, hydrochloride, HCl, ghrelin, receptors, antagonists, GHS-R1a, GHSR, Ghrelin, Receptors, 3959, Tocris Bioscience
4 Citations for YIL 781 hydrochloride
Citations are publications that use Tocris products. Selected citations for YIL 781 hydrochloride include:
Tóth et al (2018) Ghrelin receptor antagonism of hyperlocomotion in cocaine-sensitized mice requires βarrestin-2. Synapse 72 PMID: 28941296
Song et al (2013) Ghrelin modulates lateral amygdala neuronal firing and blocks acquisition for conditioned taste aversion. PLoS One 8 e65422 PMID: 23762368
Marc G et al (2019) Encoding the β-Arrestin Trafficking Fate of Ghrelin Receptor GHSR1a: C-Tail-Independent Molecular Determinants in GPCRs. ACS Pharmacol Transl Sci 2 230-246 PMID: 32259059
Evron et al (2014) G Protein and β-arrestin signaling bias at the ghrelin receptor. J Biol Chem 289 33442 PMID: 25261469
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.